4-氯-1H-吡唑并[3,4-d]嘧啶合成路线 （共 23 条）
反应条件
triethylamine; hydrazine in 1,4-dioxane T=20°C; 1 h;
参考文献
Sunesis Pharmaceuticals, Inc
Patent: US2009/5359 A1, 2009 ;
Location in patent: Page/Page column 18 ;
US 20090005359 A1
反应条件
1: With N-ethyl-N,N-diisopropylamine; trichlorophosphate in toluene T=80°C; 2 h; 2: With dipotassium hydrogenphosphate in water; toluene T=4 - 20°C;
参考文献
ELI LILLY AND COMPANY
Patent: WO2008/140947 A1, 2008 ;
Location in patent: Page/Page column 36-37 ;
WO 2008/140947 A1
反应条件
1: 4,6-dichloro-pyrimidine-5-carboxaldehyde With triethylamine in tetrahydrofuran T=0°C; 0.166667 h; Inert atmosphere; 2: hydrazine hydrate in tetrahydrofuran T=0 - 20°C; 1 h; Inert atmosphere;
参考文献
Morrill, Christie; Babu, Suresh; Almstead, Neilg.; Moon, Young-Choon
Synthesis (Germany), 2013 , vol. 45, # 13 art. no. SS-2013-C0248-OP, p. 1791 - 1806
反应条件
1: 4,6-dichloro-pyrimidine-5-carboxaldehyde With triethylamine in tetrahydrofuran T=0°C; 0.166667 h; Inert atmosphere; 2: hydrazine monohydrochloride in tetrahydrofuran T=20°C; 1 h; Inert atmosphere;
参考文献
Babu, Suresh; Morrill, Christie; Almstead, Neil G.; Moon, Young-Choon
Organic Letters, 2013 , vol. 15, # 8 p. 1882 - 1885
反应条件
trichlorophosphate in N,N-dimethyl-formamide 12 h; RefluxInert atmosphere;
参考文献
Tetrahedron Letters, , vol. 54, # 38 p. 5204 - 5206
反应条件
N-iodo-succinimide in N,N-dimethyl-formamide T=50°C; 16 h;
参考文献
ELI LILLY AND COMPANY
Patent: WO2008/140947 A1, 2008 ;
Location in patent: Page/Page column 38 ;
WO 2008/140947 A1
反应条件
N-bromosuccinmide in acetonitrile T=100°C; 0.166667 h; microwave irradiation;
参考文献
Wu, Tom Y. H.; Schultz, Peter G.; Ding, Sheng
Organic Letters, 2003 , vol. 5, # 20 p. 3587 - 3590
反应条件
di-isopropyl azodicarboxylate; triphenylphosphine in tetrahydrofuran T=0°C; Mitsunobu reaction; 1 h;
参考文献
Braendvang, Morten; Gundersen, Lise-Lotte
Tetrahedron Letters, 2007 , vol. 48, # 17 p. 3057 - 3059
反应条件
N-ethyl-N,N-diisopropylamine in 1-methyl-pyrrolidin-2-one T=80°C;
参考文献
ARRAY BIOPHARMA INC.
Patent: WO2005/51304 A2, 2005 ;
Location in patent: Page/Page column 162-163 ;
WO 2005/051304 A2
参考文献
Robins
Journal of the American Chemical Society, 1956 , vol. 78, p. 784,787
Journal of the American Chemical Society, 1957 , vol. 79, p. 6407,6413
